dc.contributor.author | Cikla, Pelin | |
dc.contributor.author | Ozsavci, Derya | |
dc.contributor.author | Bingol-Ozakpinar, Ozlem | |
dc.contributor.author | Sener, Azize | |
dc.contributor.author | Cevik, Ozge | |
dc.contributor.author | Ozbas-Turan, Suna | |
dc.contributor.author | Akbuga, Julide | |
dc.contributor.author | Sahin, Fikrettin | |
dc.contributor.author | Kucukguzel, S. Guniz | |
dc.date.accessioned | 2019-07-27T12:10:23Z | |
dc.date.accessioned | 2019-07-28T09:59:55Z | |
dc.date.available | 2019-07-27T12:10:23Z | |
dc.date.available | 2019-07-28T09:59:55Z | |
dc.date.issued | 2013 | |
dc.identifier.issn | 0365-6233 | |
dc.identifier.uri | https://dx.doi.org/10.1002/ardp.201200449 | |
dc.identifier.uri | https://hdl.handle.net/20.500.12418/8720 | |
dc.description | WOS: 000318810800005 | en_US |
dc.description | PubMed ID: 23609809 | en_US |
dc.description.abstract | Etodolac hydrazide and a novel series of etodolac hydrazide-hydrazones 315 and etodolac 4-thiazolidinones 1626 were synthesized in this study. The structures of the new compounds were determined by spectral (FT-IR, 1H NMR, 13C NMR, HREI-MS) methods. Some selected compounds were determined at one dose toward the full panel of 60 human cancer cell lines by the National Cancer Institute (NCI, Bethesda, USA). 2-(1,8-Diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-yl)acetic acid[(4-chlorophenyl)methylene]hydrazide 9 demonstrated the most marked effect on the prostate cancer cell line PC-3, with 58.24% growth inhibition at 105M (10 mu M). Using the MTT colorimetric method, compound 9 was evaluated in vitro against the prostate cell line PC-3 and the rat fibroblast cell line L-929, for cell viability and growth inhibition at different doses. Compound 9 exhibited anticancer activity with an IC50 value of 54 mu M (22.842 mu g/mL) against the PC-3 cells and did not display any cytotoxicity toward the L-929 rat fibroblasts, compared to etodolac. In addition, this compound was evaluated for caspase-3 and Bcl-2 activation in the apoptosis pathway, which plays a key role in the treatment of cancer. | en_US |
dc.description.sponsorship | Scientific and Technical Research Council of Turkey (TUBITAK) [SBAG-HYD-339 (108S257)] | en_US |
dc.description.sponsorship | This research was supported by The Scientific and Technical Research Council of Turkey (TUBITAK), Research Fund Project Number: SBAG-HYD-339 (108S257). The authors are grateful to Dr. Jurgen Gross from the Institute of Organic Chemistry, University of Heidelberg, for his generous help on obtaining HR-EI/FAB mass spectra of the synthesized compounds. We thank the Division of Cancer Research, National Cancer Institute, Bethesda, MD, USA, for the anticancer activity screening. Etodolac was supplied by Bilim Pharmaceutical Industry Inc. | en_US |
dc.language.iso | eng | en_US |
dc.publisher | WILEY-V C H VERLAG GMBH | en_US |
dc.relation.isversionof | 10.1002/ardp.201200449 | en_US |
dc.rights | info:eu-repo/semantics/closedAccess | en_US |
dc.subject | Apoptosis | en_US |
dc.subject | Etodolac | en_US |
dc.subject | Hydrazide-hydrazone | en_US |
dc.subject | PC-3 prostate cancer cell line | en_US |
dc.subject | 4-Thiazolidinone | en_US |
dc.title | Synthesis, Cytotoxicity, and Pro-Apoptosis Activity of Etodolac Hydrazide Derivatives as Anticancer Agents | en_US |
dc.type | article | en_US |
dc.relation.journal | ARCHIV DER PHARMAZIE | en_US |
dc.contributor.department | [Cikla, Pelin -- Kucukguzel, S. Guniz] Marmara Univ, Dept Pharmaceut Chem, TR-34668 Istanbul, Turkey -- [Ozsavci, Derya -- Bingol-Ozakpinar, Ozlem -- Sener, Azize -- Cevik, Ozge] Marmara Univ, Dept Biochem, TR-34668 Istanbul, Turkey -- [Cevik, Ozge] Cumhuriyet Univ, Dept Biochem, Sivas, Turkey -- [Ozbas-Turan, Suna -- Akbuga, Julide] Marmara Univ, Dept Pharmaceut Biotechnol, TR-34668 Istanbul, Turkey -- [Sahin, Fikrettin] Yeditepe Univ, Dept Genet & Bioengn, Istanbul, Turkey | en_US |
dc.contributor.authorID | Cevik, Ozge -- 0000-0002-9325-3757 | en_US |
dc.identifier.volume | 346 | en_US |
dc.identifier.issue | 5 | en_US |
dc.identifier.endpage | 379 | en_US |
dc.identifier.startpage | 367 | en_US |
dc.relation.publicationcategory | Makale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanı | en_US |